Assay Detail

CHEMBL5049720

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding

Inhibition of GAK (unknown origin)

ChEMBL ↗

Free Research Context This assay will appear in recent viewed items on this browser. Open the demo workspace to preview project-only review queues.

Research home Demo workspace

Target

Cyclin-G-associated kinase (CHEMBL4355) ↗

Open DB target context

Use one target anchor to keep assay intent, target linkage, and tested compound review aligned.

Loading context

Cyclin-G-associated kinase (CHEMBL4355) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Cyclin-G-associated kinase

CHEMBL4355

Anchored from Assay target.

Protein identity Cyclin-G-associated kinase

Disease frame Disease evidence pending

Open the live target snapshot or evidence card before reviewing assay metadata so target fit and disease framing stay reusable.

Review focus Open DB context pending

Open the live target snapshot before relying on this target frame across surface handoff.

Open target snapshot Open evidence card Search with this context

Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Cyclin-G-associated kinase (CHEMBL4355) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of (<i>S</i>)-1-((2',6-Bis(difluoromethyl)-[2,4'-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein-2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain.

Luo G, Chen L, Kostich WA, Hamman B, Allen J, Easton A, Bourin C, Gulianello M, Lippy J, Nara S, Maishal TK, Thiyagarajan K, Jalagam P, Pattipati SN, Dandapani K, Dokania M, Vattikundala P, Sharma V, Elavazhagan S, Verma MK, Das ML, Wagh S, Balakrishnan A, Johnson BM, Santone KS, Thalody G, Denton R, Saminathan H, Holenarsipur VK, Kumar A, Rao A, Putlur SP, Sarvasiddhi SK, Shankar G, Louis JV, Ramarao M, Conway CM, Li YW, Pieschl R, Tian Y, Hong Y, Ditta J, Mathur A, Li J, Smith D, Pawluczyk J, Sun D, Yip S, Wu DR, Vetrichelvan M, Gupta A, Wilson A, Gopinathan S, Wason S, Bristow L, Albright CF, Bronson JJ, Macor JE, Dzierba CD.
J Med Chem (2022) 65 : 4457 -4480
PubMed 35257579 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	6.62	7.14

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL5088205	—	—	1	7.14
CHEMBL5089410	PILAVAPADIN	2.0	1	6.10

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL5088205	—	IC50	=	73.0	nM	7.14
CHEMBL5089410	PILAVAPADIN	IC50	=	800.0	nM	6.10